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Journal of
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Maroof et al., J Bioequiv Availab 2015, 7:1

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DOI: 10.4172/jbb.1000214

ailabilit
Bioequivalence & Bioavailability
Jo

ISSN: 0975-0851 y

Review Article Open


OpenAccess
Access

Flurbiprofen: A Potent Pain Reliever


Maroof K1, Zafar F1, Ali H1 and Naveed S2*
1
Faculty of Pharmacy, Ziauddin University, Karachi, Pakistan
2
Jinnah University for Women, Karachi, Pakistan

Abstract
Flurbiprofen, a non-steroidal anti-inflammatory analgesic drug is a phenylalkanoic acid derivative. It is used in
degenerative joint disease, rheumatoid arthritis, allied conditions and ankylosing spondylitis. In this review article we
have compile its chemistry pharmacokinetic study, dose mode of action and its uses.

Keywords: Flurbiprofen; Pharmacokinetics; Dose Indications


Chemistry Flurbiprofen tablets are used in the management of acute or long-
term treatment of osteoarthritis, rheumatoid arthritis, joint stiffness
Flurbiprofen, a non steroidal anti-inflammatory drug is a and dysmenorrhea [17,18] gout, ankylosing spondylitis, periodontitis,
phenylalkanoic acid derivative (2-2-Fluoro-4-biphenyl 4-yl, propionic reduction postoperative pain, propofol injection pain, and in initial
acid) having molecular weight 244.3 g/mol with molecular formula of treated pain induced from cancer,Topical ophthalmic flurbiprofen
C15H13FO2 [1-3] . Flurbiprofen is commercially available as a racemate preparations are also used to prevent intraoperative miosis [19].
blend of (+) Sand (-) R-enantiomers. The enanteomeric form of the
drug has potentially developing role in the treatment of Alzheimer’s
Dosage Forms
disease and metastatic prostate cancer with anti-inflammatory activity It is available as 50 mg and 100 mg tablets and also as 0.03%
[4-5]. Davis et al in 2000 observed the significant stimulatory effects on ophthalmic solution [20]. Micro and nano emulsions are also reported
intestinal permeability in rats followed single oral doses of Flurbiprofen in literature.
as racemate and enantiomer [6] (Figure 1). Drug Interactions
Pharmacokinetics Flurbiprofen is shown to interact with Quinolone antacids,
Aetaminophen, Fluconazole, Dapsone and Insulin [21-27].
Flurbiprofen completely absorbed after oral administration [7] with
Significant increase in toxicities of warfarin (anticoagulants), Lithium,
peak plasma levels occurring at 1 hour Plasma concentration is related
Methotrexate and Cyclosporine are reported with Flurbiprofen.
to dosage in the range 15 to 150 mg and peak plasma concentration
Reduction in urinary volume, sodium, and potassium concentration
is about 12μg/ml after a 100 mg dose and is usually attained 1.5 to 3 is also reported with concomitant use of furosemide and Flurbiprofen.
hours after ingestion [8,9]. Flurbiprofen is 99% bound to human serum
albumin [10,11]. Flurbiprofen undergoes rapid oxidative metabolism Other Interactions
and is excreted primarily in the urine as both glucuronide and
Grape and cranberry juice significantly alters the drug clearance
sulphate conjugates and approx 20% of drug eliminated unchanged
[10,11]. There are no known active metabolites in humans and there
is no evidence of dose dependent alterations of pharmacokinetics or
of drug accumulation in plasma after multiple dose administration.
The elimination half-life is about 3.5 hours during repeated doses
[12]. Gastric emptying rate is found notably higher in fed state [13].
Flurbiprofen is a CYP2C9 substrate and modification of the Dose
adjustments are recommended when given with inhibitor of CYP2C9
agents [14]. Flurbiprofen gastrointestinal tolerance is considered better
than other NSAIDs i.e. indomethacin and aspirin, and comparable to
naproxen and ibuprofen. It has shown no problematic or irreversible
Figure 1: Structure of flurbiprofen.
hepatotoxic, carcinogenic or teratogenic effects. Hypertensive and
renal effects are probably similar to other NSAIDs.

Dose
*Corresponding author: Naveed S, Jinnah University for Women, Karachi,
150-200 mg dose is recommended daily. 300 mg is the maximum Pakistan, Tel: 0300-2621917; E-mail: safila117@yahoo.com
daily dose. Drug should administer with food to prevent stomach upset Received October 10, 2014; Accepted December 30, 2014; Published January
[15]. 02, 2015

Citation: Maroof K, Zafar F, Ali H, Naveed S (2015) Flurbiprofen: A Potent Pain


Mechanism of Action: (Rephrase) Reliever. J Bioequiv Availab 7: 056-058. doi:10.4172/jbb.1000214

Flurbiprofen inhibits the enzyme (cyclooxygenase I and Copyright: © 2015 Maroof K, et al. This is an open-access article distributed under
the terms of the Creative Commons Attribution License, which permits unrestricted
cyclooxygenase II) the makes prostaglandins which results in the
use, distribution, and reproduction in any medium, provided the original author and
valuable reduction in the concentrations of prostaglandins [16]. source are credited.

J Bioequiv Availab
ISSN: 0975-0851 JBB, an open access journal Volume 7(1): 056-058 (2015) - 56
Citation: Maroof K, Zafar F, Ali H, Naveed S (2015) Flurbiprofen: A Potent Pain Reliever. J Bioequiv Availab 7: 056-058. doi:10.4172/jbb.1000214

while pomegranate and blurberry showed no pharmacokinetic polymorphism on the metabolism of flurbiprofen in vitro. Drug Dev Ind Pharm
21: 1-5.
interaction with flurbiprofen [28-32].
12. Stefan O (2008) Encyclopedia of Molecular Pharmacology 2nd (Edn.) Springer
Side Effects 1: 875

Serious effects are dose related including ulcerations, burning, 13. Dressman JB, Berardi RR, Elta GH, Gray TM, Montgomery PA (1992)
Absorption of flurbiprofen in the fed and fasted states. Pharm Res 9: 901-907
cramps, nausea, gastritis. GI bleeding, and liver toxicity is also reported
with long term use. Rare effects range from Rash, ringing in the ears to 14. Mano Y, Usui T, Kamimura H (2007) Predominant contribution of UDP-
glucuronosyltransferase 2B7 in the glucuronidation of racemic flurbiprofen in
lightheadedness [28]. the human liver. Drug Metab Dispos 35: 1182-1187.

Caution 15. Mano N, Nikaido A, Narui T, Yamasaki D, Goto J (2002) Rapid and simple
quantitative assay method for diastereomeric flurbiprofen glucuronides in the
Risk of upper gastrointestinal ulcer, asthma, heart failure, incubation mixture. J Chromatogr B Analyt Technol Biomed Life Sci 776: 125-
hives, impaired kidney function patients associated with selective 131.
cyclooxygenase inhibitors. 16. Geisslinger G, Schaible HG (1996) New insights into the site and mode of
antinociceptive action of flurbiprofen enantiomers. J Clin Pharmacol 36: 513-
Pregnancy and Lactation 520.
17. Ashraf Mozayani (2012) Handbook of Drug Interactions: A Clinical and Forensic
Flurbiprofen is contraindicated in pregnancy and also nursing. Guide, 2nd (Edn) Humana press: 438-440.

Overdose 18. McAdam BF, Catella-Lawson F, Mardini IA, Kapoor S, Lawson JA, et al. (1999)
Systemic biosynthesis of prostacyclin by cyclooxygenase (COX)-2: the human
Overdose symptoms include nausea, stomach pain, vomiting, pharmacology of a selective inhibitor of COX-2. Proc Natl Acad Sci U S A 96:
drowsiness, dizziness, less urination, problem breathing, and fainting 272-277.
[12,21]. 19. Eriksen JL, Sagi SA, Smith TE, Weggen S, Das P, et al. (2003) NSAIDs and
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and codeine in post-operative dental pain [33-37]. Flurbiprofen axetil
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used to decrease the pain at the site of injection. However, flurbiprofen
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Citation: Maroof K, Zafar F, Ali H, Naveed S (2015) Flurbiprofen: A Potent Pain Reliever. J Bioequiv Availab 7: 056-058. doi:10.4172/jbb.1000214

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